Radioligand · neuroendocrine tumors
Lutetium Lu-177 dotatate (Lutathera) is a radioactive drug that homes in on tumors carrying somatostatin receptors. It joins a somatostatin-like peptide to the radioactive metal lutetium-177, carrying radiation to the tumor cells. It is given by intravenous infusion, with precautions to limit radiation exposure, for gastroenteropancreatic neuroendocrine tumors.
Many neuroendocrine tumors carry somatostatin receptors, especially subtype 2 (SSTR2). The drug's peptide part, dotatate, is a somatostatin analog that binds SSTR2 most strongly, while a chemical cage holds the radioactive lutetium-177 atom. Once bound to a receptor, the complex is taken inside the cell. Lutetium-177 then emits beta radiation, which damages cells through free radicals, affecting both the receptor-positive tumor cell and cells nearby1. It is used only for tumors shown to be receptor-positive.
An amino-acid infusion is given alongside; in studies it cut the median radiation dose to the kidneys by about half (47%)1.
NETTER-1 randomized 229 people with advanced, progressing, receptor-positive midgut neuroendocrine tumors to Lu-177 dotatate plus standard octreotide or to high-dose octreotide alone. At 20 months, an estimated 65% versus 11% were alive without progression, and objective tumor responses occurred in 18% versus 3%2. The final analysis, however, did not show a statistically significant overall survival gain (median 48 vs 36 months), and 2 of 111 treated patients developed myelodysplastic syndrome during long-term follow-up3. NETTER-2 studied it as first treatment in 226 people with newly diagnosed, higher-grade (grade 2-3) gastroenteropancreatic tumors: median progression-free survival was 22.8 months versus 8.5 months with high-dose octreotide4.
The FDA approved lutetium Lu-177 dotatate in 2018 as Lutathera for somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors, including foregut, midgut and hindgut tumors; the label now covers adults and children 12 and older1. A second brand, Bexlutry, was approved in 2026 for adults with the same tumors5.
Per the FDA label, the most common severe (grade 3-4) effects were low lymphocyte counts, raised liver enzymes, vomiting, nausea, high blood sugar and low potassium. Warnings cover radiation exposure, bone-marrow suppression, later myelodysplastic syndrome and leukemia (median onset 29 and 55 months), kidney and liver toxicity, hypersensitivity, neuroendocrine hormonal crises (flushing, diarrhea, low blood pressure), fetal harm and possible infertility1.
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